acetylcysteine, Acetadote, Cetylev

 Classification 

Therapeutic: antidotes (for acetaminophen toxicity), mucolytic

Indications

PO, IV: Antidote for the management of potentially

hepatotoxic overdose of acetaminophen. Inhaln: Mucolytic

in the management of conditions associated with

thick viscid mucous secretions. Unlabeled Use: PO:

Prevention of radiocontrast-induced renal dysfunction.

Action

PO, IV: Decreases the buildup of a hepatotoxic metabolite

in acetaminophen overdosage. Inhaln: Degrades

mucus, allowing easier mobilization and expectoration.

Therapeutic Effects: PO: Prevention or lessening

of liver damage following acetaminophen overdose. Inhaln:

Lowers the viscosity of mucus.

Pharmacokinetics

Absorption: Absorbed from the GI tract following

oral administration. Action is local following inhalation;

remainder may be absorbed from pulmonary epithelium.

IV administration results in complete bioavailability.

Distribution: Crosses the placenta; 0.47 L/kg.

Protein Binding: 83% bound to plasma proteins.

Metabolism and Excretion: Partially metabolized

by the liver, 22% excreted renally.

Half-life: Adults—5.6 hr (qin hepatic impairment)

newborns—11 hr.

TIME/ACTION PROFILE

ROUTE ONSET PEAK DURATION

PO (antidote) unknown 30–60 min 4 hr

IV (antidote) unknown unknown unknown

Inhaln (mucolytic)

1 min 5–10 min short

Contraindications/Precautions

Contraindicated in: Hypersensitivity.

Use Cautiously in: Severe respiratory insufficiency,

asthma, or history of bronchospasm; History of GI

bleeding (oral only); OB, Lactation: Safety not established.

Adverse Reactions/Side Effects

CNS: drowsiness. CV: vasodilation, tachycardia, hypotension.

EENT: rhinorrhea. Resp: bronchospasm,

bronchial/tracheal irritation, chest tightness,qsecretions.

GI: nausea, vomiting, stomatitis. Derm: rash,

clamminess, pruritus, urticaria. Misc: allergic reactions

(primarily with IV), including ANAPHYLAXIS, ANGIOEDEMA,

chills, fever.

Interactions

Drug-Drug: Activated charcoal may adsorb orally

administered acetylcysteine andpits effectiveness as an

antidote.

Route/Dosage

Acetaminophen Overdose

PO (Adults and Children): 140 mg/kg initially, followed

by 70 mg/kg every 4 hr for 17 additional doses.

IV (Adults and Children): Loading dose—150 mg/ A kg (maximum: 15 g) over 60 min initially followed by First maintenance dose—50 mg/kg (maximum: 5 g) over 4 hr, then second maintenance dose—100 mg/ kg (maximum: 10 g) over 16 hr. Mucolytic Inhaln (Adults and Children 1– 12 yrs): Nebulization via face mask—3– 5 mL of 20% solution or 6– 10 mL of the 10% solution 3– 4 times daily; nebulization via tent or croupette—volume of 10– 20% solution required to maintain heavy mist; direct instillation—1– 2 mL of 10– 20% solution every 1– 4 hr; intratracheal instillation via tracheostomy—1–2 mL of 10– 20% solution every 1– 4 hr (up to 2– 5 mL of 20% solution via tracheal catheter into particular segments of the bronchopulmonary tree). Inhaln (Infants): Nebulization—1– 2 mL of 20% solution or 2– 4 mL of 10% solution 3– 4 times daily. Prevention of Radiocontrast-Induced Renal Dysfunction PO (Adults): 600 mg twice daily for 2 days, beginning the day before the procedure. Availability (generic available) Effervescent tablets (lemon-mint flavor): 500 mg, 2.5 g. Solution for inhalation: 10% (100 mg/mL), 20% (200 mg/mL). Solution for injection: 20% (200 mg/mL).

IV (Adults and Children): Loading dose—150 mg/ A

kg (maximum: 15 g) over 60 min initially followed by

First maintenance dose—50 mg/kg (maximum: 5 g)

over 4 hr, then second maintenance dose—100 mg/

kg (maximum: 10 g) over 16 hr.

Mucolytic

Inhaln (Adults and Children 1–12 yrs): Nebulization

via face mask—3–5 mL of 20% solution or 6–

10 mL of the 10% solution 3–4 times daily; nebulization

via tent or croupette—volume of 10–20% solution

required to maintain heavy mist; direct instillation—

1–2 mL of 10–20% solution every 1–4 hr;

intratracheal instillation via tracheostomy—1–2

mL of 10–20% solution every 1–4 hr (up to 2–5 mL

of 20% solution via tracheal catheter into particular

segments of the bronchopulmonary tree).

Inhaln (Infants): Nebulization—1–2 mL of 20%

solution or 2–4 mL of 10% solution 3–4 times daily.

Prevention of Radiocontrast-Induced Renal

Dysfunction

PO (Adults): 600 mg twice daily for 2 days, beginning

the day before the procedure.

Availability (generic available)

Effervescent tablets (lemon-mint flavor): 500 mg,

2.5 g. Solution for inhalation: 10% (100 mg/mL),

20% (200 mg/mL). Solution for injection: 20%

(200 mg/mL).